Luan Zhi-Lin, Huo Xiao-Xiao, Guan You-Fei, Zhang Xiao-Yan
Advanced Institute for Medical Sciences, Dalian Medical University, Dalian 116044, China.
Sheng Li Xue Bao. 2019 Apr 25;71(2):311-318.
As a member of the nuclear receptor superfamily, the pregnane X receptor (PXR) is a ligand-activated transcription factor. PXR is highly expressed in liver and intestinal tissues, and also found in other tissues and organs, such as stomach and kidney. After heterodimerization with retinoid X receptor (RXR), PXR recruits numerous co-activating factors, and binds to specific DNA response elements to perform transcriptional regulation of the downstream target genes. As an acknowledged receptor for xenobiotics, PXR was initially considered as a nuclear receptor regulating drug metabolizing enzymes and transporters. However, nowadays, PXR has also been recognized as an important endobiotic receptor. Recent studies have shown that PXR activation can regulate glucose metabolism, lipid metabolism, steroid endocrine homeostasis, detoxification of cholic acid and bilirubin, bone mineral balance, and immune inflammation in vivo. This review focuses on the role of PXR in metabolism of endogenous substances.
作为核受体超家族的一员,孕烷X受体(PXR)是一种配体激活的转录因子。PXR在肝脏和肠道组织中高度表达,在其他组织和器官如胃和肾脏中也有发现。与视黄酸X受体(RXR)异源二聚化后,PXR募集众多共激活因子,并与特定的DNA反应元件结合,以对下游靶基因进行转录调控。作为一种公认的外源性物质受体,PXR最初被认为是一种调节药物代谢酶和转运蛋白的核受体。然而,如今PXR也被认为是一种重要的内源性物质受体。最近的研究表明,PXR激活可在体内调节葡萄糖代谢、脂质代谢、类固醇内分泌稳态、胆酸和胆红素解毒、骨矿物质平衡以及免疫炎症。本综述重点关注PXR在内源性物质代谢中的作用。